Therapeutic perspective of thiosemicarbazones derivatives in inflammatory pathologies: A summary of in vitro/in vivo studies

Int Immunopharmacol. 2021 Jul:96:107778. doi: 10.1016/j.intimp.2021.107778. Epub 2021 May 24.

Abstract

Following induction of inflammation, the nuclear factor kappa B (NF-κB) in activated macrophages induces the transcription of pro-inflammatory cytokines such as tumor necrosis factor-alpha (TNF-α), interleukin-1β (IL-1β), interleukin-6 (IL-6), and cyclooxygenase (COX), an inflammatory enzyme implicated in the synthesis of prostaglandins (PGs). The latter are involved in the transition and the maintenance of chronic inflammation underling various chronic disorders that require treatment. Concerning this, many anti-inflammatory drugs are available to treat the inflammatory disorders, but their therapeutic use is associated with a variety of side effects. Therefore, the discovery of new safer and potential anti-inflammatory drugs is necessary. In this regard, thiosemicarbazones (TSC) compounds and their metals complexes attracted high interest due to their wide range of biological activities, interestingly, the anti-inflammatory activity. They are formed by the action of thiosemicarbazide on an aldehyde or ketone, and contain a sulfur atom in place of the oxygen atom. Their ability to form a stable complex with transition metal is known to enhances the biological activity and reduces the side effects of the parent compound. Thus, this review article describes the inflammatory response mediated by NF-κB-COX-PGs and summarizes the anti-inflammatory activity of different thiosemicarbazones derivatives synthesized in research area.

Keywords: Anti-inflammatory activity; Chronic inflammation; Cyclooxygenase; Nuclear factor kappa B; Prostaglandins; Thiosemicarbazones.

Publication types

  • Review

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / chemistry*
  • Anti-Inflammatory Agents / pharmacology*
  • Anti-Inflammatory Agents / therapeutic use
  • Inflammation / drug therapy*
  • Inflammation / metabolism*
  • NF-kappa B / metabolism
  • Prostaglandin-Endoperoxide Synthases / metabolism
  • Prostaglandins / metabolism
  • Thiosemicarbazones / chemistry*
  • Thiosemicarbazones / pharmacology*
  • Thiosemicarbazones / therapeutic use

Substances

  • Anti-Inflammatory Agents
  • NF-kappa B
  • Prostaglandins
  • Thiosemicarbazones
  • Prostaglandin-Endoperoxide Synthases